387827-19-2Relevant articles and documents
BRAF DEGRADERS
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, (2022/02/06)
Present invention provides compounds that cause specifically the degradation of BRAF. The present compounds are useful for the treatment of various cancers.
TARGETED PROTEIN DEGRADATION
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, (2020/07/14)
This invention provides pharmaceutical protein degraders and E3 ubiquitin ligase binders for therapeutic applications as described further herein.
Practical synthesis of pharmaceutically relevant molecules enriched in sp3 character
Campbell, Peter S.,Jamieson, Craig,Simpson, Iain,Watson, Allan J. B.
, p. 46 - 49 (2017/12/27)
The expedient synthesis of compounds enriched in sp3 character is key goal in modern drug discovery. Herein, we report how a single pot Suzuki-Miyaura-hydrogenation can be used to furnish lead and fragment-like products in good to excellent yields. The approach has been successfully applied in formats amenable to parallel synthesis, in an asymmetric sense, and in the preparation of molecules with annotated biological activity.
Pyrimidine derivative, preparation method therefor and application thereof in medicine
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Paragraph 0204; 0214; 0215; 0216; 0217; 0218, (2016/10/07)
The invention relates to a pyrimidine derivative, a preparation method therefor and an application thereof in medicine. Particularly, the invention relates to a compound as shown in general formula (M) or a stereisomer, an aquo-complex, a metabolic product, a solvate, a pharmaceutically acceptable salt, a co-crystallization or a prodrug thereof; the preparation method thereof; and the application of the medicine composition thereof and the compound medicine compound in the medicine, particularly the application as an EGFR target spot inhibitor, wherein the definition of each substituent group in the general formula (M) is the same as that of the specification.
PREPARATION AND USES OF 1,2,4-TRIAZOLO [1,5a] PYRIDINE DERIVATIVES
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Page/Page column 260, (2010/12/29)
This application relates to compounds of the general Formula I and salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of treatment of hyperproliferative diseases or disorders.
Arylthiobenzylpiperidine derivatives
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Page/Page column 12, (2010/10/20)
This invention is directed to Arylthiobenzylpiperidine derivatives which are ligands at the MCH1 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the subject invention. This invention also provides a method of treating a subject suffering from obesity which comprises administering to the subject an amount of a compound of the subject invention.
MEDICINAL USE OF RECEPTOR LIGANDS
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Page/Page column 37, (2008/06/13)
Compounds of formula (I) are ligands of the melanin concentrating hormone-1 receptor (MCH-1 R), useful in the treatment of diseases responsive to modulation of melanin concentrating hormone (MCH) activity, for example feeding disorders and diseases for which obesity is a risk factor (I): wherein ring B is selected from specific substituted phenyl or benz-fused 5-membered N-containing heterocycles defined in the specification; R, is attached to a ring carbon of ring B, and represents hydrogen, F, Cl, or -OCH3; X is =CH- or =N-; L, is -CH2- or -CH2CH2- ; L2 is a bond, -CH2- or -CO-; R2 is H or C,-C3 alkyl, or -N(R2) L,- is selected from specific cyclic amino linker radicals as defined in the specification; ring A is selected from specific N- containing heterocyclic rings as defined in the specification.
4-Aryl piperidines
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Page/Page column 8, (2010/02/12)
This invention is directed to 4-aryl piperidines and related heterocyclic compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject''s depression and/or anxiety.
4-aryl piperidines
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Page/Page column 4; 9, (2010/02/12)
This invention is directed to 4-aryl piperidines and related heterocyclic compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.
DNA encoding a human melanin concentrating hormone receptor (MCH1) and uses thereof
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, (2008/06/13)
This invention provides an isolated nucleic acid encoding a human MCH1 receptor, a purified human MCH1 receptor, vectors comprising isolated nucleic acid encoding a human MCH1 receptor, cells comprising such vectors, antibodies directed to a human MCH1 receptor, nucleic acid probes useful for detecting nucleic acid encoding human MCH1 receptors, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding human MCH1 receptors, transgenic, nonhuman animals which express DNA encoding a normal or mutant human MCH1 receptor, methods of isolating a human MCH1 receptor, methods of treating an abnormality that is linked to the activity of a human MCH1 receptor, as well as methods of determining binding of compounds to mammalian MCH1 receptors. This invention further provides a method of treating a subject suffering from urinary incontinence which comprises administering to the subject an amount of an MCH1 antagonist effective to treat the subject's urinary incontinence.